CY1125060T1 - NEW BENZAMIDE DERIVATIVES AS PPAR-GAMMA REGULATORS - Google Patents

NEW BENZAMIDE DERIVATIVES AS PPAR-GAMMA REGULATORS

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Publication number
CY1125060T1
CY1125060T1 CY20221100197T CY221100197T CY1125060T1 CY 1125060 T1 CY1125060 T1 CY 1125060T1 CY 20221100197 T CY20221100197 T CY 20221100197T CY 221100197 T CY221100197 T CY 221100197T CY 1125060 T1 CY1125060 T1 CY 1125060T1
Authority
CY
Cyprus
Prior art keywords
diseases
ppar
gamma
regulators
benzamide derivatives
Prior art date
Application number
CY20221100197T
Other languages
Greek (el)
Inventor
Julio Castro-Palomino Laria
Juan CAMACHO GÓMEZ
Rodolfo RODRÍGUEZ IGLESIAS
Original Assignee
Medibiofarma, S.L.
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Medibiofarma, S.L. filed Critical Medibiofarma, S.L.
Publication of CY1125060T1 publication Critical patent/CY1125060T1/en

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D213/00Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D213/72Nitrogen atoms
    • C07D213/75Amino or imino radicals, acylated by carboxylic or carbonic acids, or by sulfur or nitrogen analogues thereof, e.g. carbamates
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/04Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/444Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/496Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/50Pyridazines; Hydrogenated pyridazines
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53771,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C255/00Carboxylic acid nitriles
    • C07C255/49Carboxylic acid nitriles having cyano groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton
    • C07C255/57Carboxylic acid nitriles having cyano groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton containing cyano groups and carboxyl groups, other than cyano groups, bound to the carbon skeleton
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D237/00Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings
    • C07D237/02Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings
    • C07D237/06Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
    • C07D237/10Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D237/20Nitrogen atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D295/00Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
    • C07D295/16Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms acylated on ring nitrogen atoms
    • C07D295/18Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms acylated on ring nitrogen atoms by radicals derived from carboxylic acids, or sulfur or nitrogen analogues thereof
    • C07D295/182Radicals derived from carboxylic acids
    • C07D295/192Radicals derived from carboxylic acids from aromatic carboxylic acids
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/04Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Pyridine Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

Η παρούσα εφεύρεση αναφέρεται σε καινοτόμα παράγωγα του χημικού τύπου (Ι) ως ρυθμιστές των PPAR-γάμμα, σε διαδικασίες για τη παρασκευή τους, σε φαρμακευτικές συνθέσεις που περιέχουν τις εν λόγω ενώσεις και στην εν λόγω ένωση για χρήση της στη θεραπεία παθολογικών καταστάσεων, διαταραχών ή νοσημάτων που μπορούν να βελτιωθούν με ρύθμιση του PPAR-γάμμα υποδοχέα, όπως είναι ο καρκίνος, μεταβολικά νοσήματα, φλεγμονώδη νοσήματα, αναπνευστικά νοσήματα, αυτοάνοσα νοσήματα, νευροεκφυλιστικά νοσήματα, καρδιαγγειακά νοσήματα και νεφρικά νοσήματα.The present invention relates to novel derivatives of the chemical formula (I) as regulators of PPAR-gamma, to processes for their preparation, to pharmaceutical compositions containing said compounds and to said compound for use in the treatment of pathological conditions, disorders or diseases that can be improved by modulating the PPAR-gamma receptor, such as cancer, metabolic diseases, inflammatory diseases, respiratory diseases, autoimmune diseases, neurodegenerative diseases, cardiovascular diseases and kidney diseases.

CY20221100197T 2017-12-12 2022-03-09 NEW BENZAMIDE DERIVATIVES AS PPAR-GAMMA REGULATORS CY1125060T1 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP17382845.0A EP3498694A1 (en) 2017-12-12 2017-12-12 New benzamide derivatives as ppar-gamma modulators
PCT/EP2018/084290 WO2019115498A1 (en) 2017-12-12 2018-12-11 New benzamide derivatives as ppar-gamma modulators

Publications (1)

Publication Number Publication Date
CY1125060T1 true CY1125060T1 (en) 2023-06-09

Family

ID=60673764

Family Applications (1)

Application Number Title Priority Date Filing Date
CY20221100197T CY1125060T1 (en) 2017-12-12 2022-03-09 NEW BENZAMIDE DERIVATIVES AS PPAR-GAMMA REGULATORS

Country Status (21)

Country Link
US (1) US11267808B2 (en)
EP (2) EP3498694A1 (en)
JP (1) JP7212235B2 (en)
KR (1) KR102688870B1 (en)
CN (1) CN111630030B (en)
AU (1) AU2018382461B2 (en)
BR (1) BR112020011558A2 (en)
CA (1) CA3084879A1 (en)
CY (1) CY1125060T1 (en)
DK (1) DK3724165T3 (en)
EA (1) EA202091433A1 (en)
ES (1) ES2908938T3 (en)
HR (1) HRP20220329T1 (en)
HU (1) HUE058004T2 (en)
LT (1) LT3724165T (en)
MX (1) MX2020006235A (en)
PL (1) PL3724165T3 (en)
PT (1) PT3724165T (en)
RS (1) RS63021B1 (en)
SI (1) SI3724165T1 (en)
WO (1) WO2019115498A1 (en)

Families Citing this family (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2021092262A1 (en) * 2019-11-05 2021-05-14 Dermira, Inc. Mrgprx2 antagonists and uses thereof
KR20230107291A (en) * 2020-11-09 2023-07-14 에자이 알앤드디 매니지먼트 가부시키가이샤 PPARγ modulators and methods of use
CN113350346B (en) * 2021-06-01 2023-06-27 广西医科大学第一附属医院 Use of vincristine in preventing or treating myocardial fibrosis
AU2023231613A1 (en) * 2022-03-08 2024-09-05 Flare Therapeutics Inc. Pparg inverse agonists and uses thereof
WO2023172846A1 (en) * 2022-03-08 2023-09-14 Flare Therapeutics Inc. Pparg inverse agonists and uses thereof
WO2023219879A1 (en) * 2022-05-09 2023-11-16 Eisai R&D Management Co., Ltd. SOLID FORM OF PPAR-gamma MODULATORS AND METHODS OF USE
CN115160341B (en) * 2022-07-18 2023-07-18 中国医学科学院医学实验动物研究所 Benzoxazine compound and pharmaceutical application thereof

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Publication number Priority date Publication date Assignee Title
US6022884A (en) 1997-11-07 2000-02-08 Amgen Inc. Substituted pyridine compounds and methods of use
PL357678A1 (en) * 2000-04-28 2004-07-26 Sankyo Company, Limited Ppargamma modulators
JP2003073357A (en) * 2001-09-03 2003-03-12 Mitsubishi Pharma Corp Rho KINASE INHIBITOR COMPRISING AMIDE COMPOUND
US20080206194A1 (en) * 2007-02-16 2008-08-28 Glazer Robert I Method for the treatment of breast cancer
US8686048B2 (en) * 2010-05-06 2014-04-01 Rhizen Pharmaceuticals Sa Immunomodulator and anti-inflammatory compounds
CN104302627A (en) * 2012-05-22 2015-01-21 北卡罗来纳大学教堂山分校 Pyrimidine compounds for the treatment of cancer

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KR102688870B1 (en) 2024-07-25
US20210171511A1 (en) 2021-06-10
EA202091433A1 (en) 2020-09-09
EP3724165B1 (en) 2022-01-12
RS63021B1 (en) 2022-04-29
JP7212235B2 (en) 2023-01-25
KR20200098557A (en) 2020-08-20
PL3724165T3 (en) 2022-04-25
EP3498694A1 (en) 2019-06-19
CN111630030B (en) 2023-06-20
PT3724165T (en) 2022-04-06
SI3724165T1 (en) 2022-06-30
MX2020006235A (en) 2020-08-24
JP2021505641A (en) 2021-02-18
DK3724165T3 (en) 2022-02-21
US11267808B2 (en) 2022-03-08
AU2018382461A1 (en) 2020-07-09
ES2908938T3 (en) 2022-05-04
LT3724165T (en) 2022-03-25
CN111630030A (en) 2020-09-04
BR112020011558A2 (en) 2020-12-08
CA3084879A1 (en) 2019-06-20
HRP20220329T1 (en) 2022-05-13
AU2018382461B2 (en) 2023-04-27
EP3724165A1 (en) 2020-10-21
HUE058004T2 (en) 2022-06-28
WO2019115498A1 (en) 2019-06-20

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